| Identification | Back Directory | [Name]
Pyrotinib Maleate | [CAS]
1397922-61-0 | [Synonyms]
SHR1258 maleate
SHR-1258 maleate
Pyrotinib Maleate
SHR-1258 dimaleate
Pyrotinib dimaleate
SHR-1258 MALEATE;SHR1258 MALEATE
2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2E)-, (2Z)-2-butenedioate (1:2) | [Molecular Formula]
C40H39ClN6O11 | [MOL File]
1397922-61-0.mol | [Molecular Weight]
815.224 |
| Hazard Information | Back Directory | [Uses]
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively[1]. | [in vivo]
Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h)[1]. | [IC 50]
HER2: 38 nM (IC50); EGFR: 13 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Li X, et al. Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X. DOI:10.1016/j.ejps.2017.01.021 |
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